Scatina J, Hicks D, Kraml M, Weidler D, Garg D, Sanda M
Clin Pharmacol Ther. 1986 May;39(5):550-3. doi: 10.1038/clpt.1986.94.
The effects of age and chronic dosing on the pharmacokinetics of the anti-inflammatory drug etodolac were evaluated in healthy young subjects, healthy elderly subjects, and elderly patients with osteoarthritis. After either single or chronic (7 days) dosing, both the healthy elderly subjects and the elderly patients with osteoarthritis had values for etodolac peak concentration, time to reach peak concentration, the AUC from 0 to 24 hours, elimination t1/2, and free fraction that did not differ significantly from those in the young (control) subjects. Despite the expected increases in the peak concentration and AUC from 0 to 24 hours for all groups after chronic dosing, there were no changes in etodolac free fraction, time to peak concentration, or t1/2. Because significant accumulation of etodolac was not observed in our elderly participants, adjustment of dosage when elderly subjects receive etodolac therapy is not indicated.
在健康年轻受试者、健康老年受试者以及患有骨关节炎的老年患者中,评估了年龄和长期给药对抗炎药物依托度酸药代动力学的影响。在单次或长期(7天)给药后,健康老年受试者和患有骨关节炎的老年患者的依托度酸峰值浓度、达峰时间、0至24小时的AUC、消除半衰期以及游离分数的值与年轻(对照)受试者相比,均无显著差异。尽管长期给药后所有组的峰值浓度和0至24小时的AUC预期会增加,但依托度酸的游离分数、达峰时间或半衰期并无变化。由于在我们的老年参与者中未观察到依托度酸的显著蓄积,因此不建议老年受试者接受依托度酸治疗时调整剂量。